| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| Other Sizes |
|
| ln Vitro |
With an IC50 of 200 and 100 nM, respectively, KP372-1 (0.0625, 0.125, 0.25, 0.5, 1.0 μM; 48 hours) suppresses the development of JMARc42 and Tu167c2 cells [1]. In Tu167c2 cells, KP372-1 (125 nM; 24 h) causes apoptosis, but in JMARc42 cells, it causes anoikis [1]. In Tu167 and JMAR cells, KP372-1 (125 nM; 30 minutes) decreases phosphorylation of S6 ribosomal protein via blocking Akt [1]. KP372-1 (IC50 = 250 nM) suppresses Akt kinase activity in JMAR cells at 0.250, 0.5, and 1.0 μM for 30 minutes [1].
|
|---|---|
| ln Vivo |
KP372-1 (10, 20 mg/kg; intravenous injection; once daily for 33 days) inhibits the growth of tumors in vivo and causes NADH oxidation without appearing to be harmful[2].
|
| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: JMARc42 and Tu167c2 cells Tested Concentrations: 0.0625, 0.125, 0.25, 0.5, 1.0 µM Incubation Duration: 48 h Experimental Results: demonstrated antiproliferative activity. Apoptosis Analysis[1] Cell Types: Tu167c2 and JMARc42 cells Tested Concentrations: 125 nM Incubation Duration: 24 h Experimental Results: Induced approximately 90% of cells apoptosis. Western Blot Analysis[1] Cell Types: Tu167 and JMAR cells Tested Concentrations: 125 nM Incubation Duration: 30 min Experimental Results: Induced a small but consistent decrease in Akt phosphorylation with a concomitant marked decrease in S6 phosphorylation. Inhibited the EGF induced phosphorylation of Aktser473 in Tu167 and AktThr308 in JMAR. Western Blot Analysis[1] Cell Types: JMAR cells Tested Concentrations: 0.250, 0.5, 1.0 µM Incubation Duration: 30 min Experimental Results: Dramatically blocked Akt kinase activity in a dose-dependent fashion, with an IC50 of 250 nM. |
| Animal Protocol |
Animal/Disease Models: Nude mice (H1299 xenografts model)[2].
Doses: 10, 20 mg/kg Route of Administration: Tailvein injection; single daily for 33 days Experimental Results: Affected tumor metabolism and suppressed tumor growth. |
| References |
[1]. Mandal M, et al. The Akt inhibitor KP372-1 inhibits proliferation and induces apoptosis and anoikis in squamous cell carcinoma of the head and neck. Oral Oncol. 2006 Apr;42(4):430-9.
[2]. Zhao Y, et al. SoNar, a Highly Responsive NAD+/NADH Sensor, Allows High-Throughput Metabolic Screening of Anti-tumor Agents. Cell Metab. 2015 May 5;21(5):777-89. [3]. Viera T, et al. DNA damage induced by KP372-1 hyperactivates PARP1 and enhances lethality of pancreatic cancer cells with PARP inhibition. Sci Rep. 2020 Nov 19;10(1):20210. |
| Molecular Formula |
C20H8N12O2
|
|---|---|
| Molecular Weight |
448.36
|
| CAS # |
1374996-60-7
|
| Related CAS # |
PDK1/Akt/Flt dual pathway inhibitor;331253-86-2
|
| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
| SMILES |
O=C1C2=CC=CC=C2C2=NN3N=NN=C3N=C12.O=C1C2=CC=CC=C2C2=NC3=NN=NN3N=C12
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: 17.86 mg/mL (39.83 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2304 mL | 11.1518 mL | 22.3035 mL | |
| 5 mM | 0.4461 mL | 2.2304 mL | 4.4607 mL | |
| 10 mM | 0.2230 mL | 1.1152 mL | 2.2304 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
